[go: up one dir, main page]

WO1998001124A2 - Preparation pharmaceutique contenant du nimesulide pour usage topique - Google Patents

Preparation pharmaceutique contenant du nimesulide pour usage topique Download PDF

Info

Publication number
WO1998001124A2
WO1998001124A2 PCT/IB1997/000816 IB9700816W WO9801124A2 WO 1998001124 A2 WO1998001124 A2 WO 1998001124A2 IB 9700816 W IB9700816 W IB 9700816W WO 9801124 A2 WO9801124 A2 WO 9801124A2
Authority
WO
WIPO (PCT)
Prior art keywords
acid
nimesulide
pharmaceutical preparation
phospholipid
pharmaceutical
Prior art date
Application number
PCT/IB1997/000816
Other languages
English (en)
Other versions
WO1998001124A3 (fr
Inventor
Paolo Luca Maria Giorgetti
Original Assignee
Errekappa Euroterapici S.P.A.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Errekappa Euroterapici S.P.A. filed Critical Errekappa Euroterapici S.P.A.
Priority to CA002231118A priority Critical patent/CA2231118C/fr
Priority to DE69711588T priority patent/DE69711588T2/de
Priority to SI9730336T priority patent/SI0853476T1/xx
Priority to JP10504989A priority patent/JPH11512116A/ja
Priority to AT97927313T priority patent/ATE215367T1/de
Priority to US09/029,456 priority patent/US5998480A/en
Priority to DK97927313T priority patent/DK0853476T5/da
Priority to EP97927313A priority patent/EP0853476B1/fr
Publication of WO1998001124A2 publication Critical patent/WO1998001124A2/fr
Publication of WO1998001124A3 publication Critical patent/WO1998001124A3/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts

Definitions

  • nimesulide (4-n ⁇ tro-2-phenoxy-methan-sulfan ⁇ hde) is a non
  • lnflammato ⁇ es such as for example, arylalkaloid acids such as acetylsahcylic
  • Nimesulide appears to be very sparingly soluble in water
  • Nimesulide's scarce water solubility and "wettability" can cause problems with drug release and constant
  • step is salification with alkaline or alkaline-earth bases This technique is not
  • bioavailability is complexation with cyclodextrins, above all ⁇ -cyclodext ⁇ ns (as
  • Another method whose widest field of application is topical administration, is to vehicle the compound by using liposomal systems consisting of
  • This invention is able to satisfy such requirement by also providing other
  • nimesulide CAS-No. 51 803-78-2
  • base of the preparation contains at
  • nimesulide can be present at concentrations from 0 1 to 15%, the phospholipid from 0.1 to 10% and the acid from 0 1 to 10% of the preparation's weight.
  • nimesulide can be present in dispersed form
  • the phospholipid can be a phosphatidyl acid ester, phosphatidylcholine in particular, and the acid can be an organic or an inorganic
  • glycol acid citric acid, aqueous hydrochloric acid.
  • the pH of the preparation according to this invention can preferably be between
  • the preparation according to this invention can contain other substances
  • the preparation according to this invention can be in the form of a gel, hpogel, cream, ointment, lotion, foam, with and without propellants or pressurized gas
  • This invention is not limited to the pharmaceutical preparation containing nimesulide as active ingredient according to the preceding description. It is
  • phospholipids do not influence nimesulide absorption.
  • the possible keratolytic activity of the organic acids is not, therefore, the primary cause of the increased absorption, but, through synergetic activity with phospholipids, it contributes towards increasing availability of a drug, such as nimesulide, that has very
  • Carboxyvinylpolymer (Carbopol 940) 2 0%

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Préparation pharmaceutique pour usage topique qui contient comme principe actif du nimesulide (CAS No 51 803-78-2) ou l'un de ses dérivés actifs. La présente invention est caractérisée par le fait que la base de ladite préparation contient au moins un phospholipide et au moins une substance à réaction acide, et spécifiquement un acide. La figure montre les résultats d'un test d'absorption de nimesulide ex vivo effectué à l'aide de formulations pour application topique, dont celles qui font l'objet de la présente invention.
PCT/IB1997/000816 1996-07-05 1997-07-02 Preparation pharmaceutique contenant du nimesulide pour usage topique WO1998001124A2 (fr)

Priority Applications (8)

Application Number Priority Date Filing Date Title
CA002231118A CA2231118C (fr) 1996-07-05 1997-07-02 Preparation pharmaceutique contenant du nimesulide pour usage topique
DE69711588T DE69711588T2 (de) 1996-07-05 1997-07-02 Nimesulid enthaltende pharmazeutische zubereitung zur topischen anwendung
SI9730336T SI0853476T1 (en) 1996-07-05 1997-07-02 Pharmaceutical preparation containing nimesulide for topical use
JP10504989A JPH11512116A (ja) 1996-07-05 1997-07-02 局所適用のためのニメスライド含有医薬
AT97927313T ATE215367T1 (de) 1996-07-05 1997-07-02 Nimesulid enthaltende pharmazeutische zubereitung zur topischen anwendung
US09/029,456 US5998480A (en) 1996-07-05 1997-07-02 Pharmaceutical preparation containing nimesulide for topical use
DK97927313T DK0853476T5 (da) 1996-07-05 1997-07-02 Nimesulidholdigt farmaceutisk præparat til topisk anvendelse
EP97927313A EP0853476B1 (fr) 1996-07-05 1997-07-02 Preparation pharmaceutique contenant du nimesulide pour usage topique

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT96RM000480A IT1291278B1 (it) 1996-07-05 1996-07-05 Preparazione farmaceutica a base di nimesulide per uso topico
ITRM96A000480 1996-07-05

Publications (2)

Publication Number Publication Date
WO1998001124A2 true WO1998001124A2 (fr) 1998-01-15
WO1998001124A3 WO1998001124A3 (fr) 1998-02-19

Family

ID=11404325

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB1997/000816 WO1998001124A2 (fr) 1996-07-05 1997-07-02 Preparation pharmaceutique contenant du nimesulide pour usage topique

Country Status (13)

Country Link
US (1) US5998480A (fr)
EP (1) EP0853476B1 (fr)
JP (1) JPH11512116A (fr)
KR (1) KR19990044280A (fr)
CN (1) CN1199335A (fr)
AT (1) ATE215367T1 (fr)
CA (1) CA2231118C (fr)
DE (1) DE69711588T2 (fr)
DK (1) DK0853476T5 (fr)
ES (1) ES2175419T3 (fr)
IT (1) IT1291278B1 (fr)
PT (1) PT853476E (fr)
WO (1) WO1998001124A2 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998037879A1 (fr) * 1997-02-25 1998-09-03 Helsinn Healthcare S.A. Systeme de gel de nimesulide a usage topique
WO2000072884A1 (fr) * 1999-05-31 2000-12-07 Dinesh Shantilal Patel Nouvelle preparation de n-(4-nitro-2-phenoxyphenyl)methanesulfonamide
EP1172101A1 (fr) * 2000-06-20 2002-01-16 Helsinn Healthcare S.A. L'utilisation de nimesulide pour le traitement du psoriasis et de l'arthrite psoriatique
EP1166779A3 (fr) * 2000-06-20 2002-05-08 Helsinn Healthcare S.A. Utilisation de nimesulide pour le traitement des maladies dermatologiques
TR200906775A1 (tr) * 2009-09-02 2011-03-21 Sanovel İlaç San.Ve Ti̇c.A.Ş. Nimesulid ve kas gevşetici kombinasyonları

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1291895B1 (it) 1997-04-24 1999-01-21 Errekappa Euroterapici S P A Preparazione farmaceutica fluida a base di nimesulide per uso orale e rinofaringeo
KR100752990B1 (ko) * 2006-08-02 2007-08-30 주식회사 대웅 나노리포좀 및 천연 추출물을 포함하는 피부 질환의 예방또는 치료용 조성물
WO2014125085A1 (fr) 2013-02-15 2014-08-21 Sanovel Ilac Sanayi Ve Ticaret A.S. Formulations pharmaceutiques orales comprenant du nimésulide et du thiocolchicoside

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR206496A1 (es) * 1972-07-03 1976-07-30 Riker Laboratories Inc Procedimiento para la preparacion de 2-fenoxi-4-nitro-alquil o haloalquilsulfonanilidas
US4933172A (en) * 1988-10-06 1990-06-12 Warner-Lambert Co. Method of and compositions for treating destructive periodontal disease
WO1991000043A1 (fr) * 1989-06-28 1991-01-10 Black & Decker Inc. Grille-pain
ES2023552A6 (es) * 1990-05-22 1992-01-16 Leetrim Limited Procedimiento para la preparacion de compuestos de inclusion de nimesulida con ciclodextrina.
IT1251838B (it) * 1991-09-20 1995-05-26 Lpb Ist Farm Uso della nimesulide nel trattamento della cataratta
IL106035A0 (en) * 1992-06-24 1993-10-20 Skyview Cooling Co Pest eradicating composition and methods for reducing pests on growing plants utilizing the same
ES2193200T3 (es) * 1994-09-27 2003-11-01 Univ Leiden Composicion acuosa libre de fosfolipidos y colesterol para la aplicacion topica sobre la piel.
MXPA97002401A (es) * 1994-10-05 2004-08-20 Helsinn Healthcare Sa Agente antiinflamatorio para uso externo.
US5763422A (en) * 1995-01-27 1998-06-09 Board Of Regents, The University Of Texas System Methods of enhancing the therapeutic activity of NSAIDS and compositions of zwitterionic phospholipids useful therein
US5654337A (en) * 1995-03-24 1997-08-05 II William Scott Snyder Topical formulation for local delivery of a pharmaceutically active agent
HUP9601442A3 (en) * 1995-07-25 1999-03-29 Panacea Biotec Ltd Nes antinflammatory and analgetic pharmaceutical compositions, containing nimesulid for transdermal use, and process for producing them
US5814659A (en) * 1996-04-23 1998-09-29 Dtr Dermal Therapy (Barbados) Inc. Topical analgesic composition
HUP9601443A3 (en) * 1996-05-29 1999-03-29 Panacea Biotec Ltd Injectable analgetic pharmaceutical compositions for intramuscular use containing nimesulid, and process for producing them
US5837289A (en) * 1996-07-23 1998-11-17 Grasela; John C. Transdermal delivery of medications using a combination of penetration enhancers
IT1286496B1 (it) * 1996-11-20 1998-07-15 Leetrim Ltd Dublin Composizione farmaceutica orale ad attivita' antipiretica,analgesica ed antiinfiammatoria

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998037879A1 (fr) * 1997-02-25 1998-09-03 Helsinn Healthcare S.A. Systeme de gel de nimesulide a usage topique
US7186755B2 (en) 1997-02-25 2007-03-06 Helsinn Health Care S.A. Nimesulide gel systems for topical use
WO2000072884A1 (fr) * 1999-05-31 2000-12-07 Dinesh Shantilal Patel Nouvelle preparation de n-(4-nitro-2-phenoxyphenyl)methanesulfonamide
EP1172101A1 (fr) * 2000-06-20 2002-01-16 Helsinn Healthcare S.A. L'utilisation de nimesulide pour le traitement du psoriasis et de l'arthrite psoriatique
EP1166779A3 (fr) * 2000-06-20 2002-05-08 Helsinn Healthcare S.A. Utilisation de nimesulide pour le traitement des maladies dermatologiques
TR200906775A1 (tr) * 2009-09-02 2011-03-21 Sanovel İlaç San.Ve Ti̇c.A.Ş. Nimesulid ve kas gevşetici kombinasyonları
EP2292218A3 (fr) * 2009-09-02 2011-07-27 Sanovel Ilac Sanayi ve Ticaret A.S. Nimesulide et ses combinaisons pour le relâchement musculaire

Also Published As

Publication number Publication date
DE69711588T2 (de) 2002-10-31
US5998480A (en) 1999-12-07
EP0853476A2 (fr) 1998-07-22
DK0853476T3 (da) 2002-07-29
PT853476E (pt) 2002-08-30
CN1199335A (zh) 1998-11-18
KR19990044280A (ko) 1999-06-25
WO1998001124A3 (fr) 1998-02-19
DE69711588D1 (de) 2002-05-08
IT1291278B1 (it) 1999-01-07
CA2231118A1 (fr) 1998-01-15
ITRM960480A1 (it) 1998-01-05
CA2231118C (fr) 2001-09-18
DK0853476T5 (da) 2002-10-07
JPH11512116A (ja) 1999-10-19
ES2175419T3 (es) 2002-11-16
ATE215367T1 (de) 2002-04-15
ITRM960480A0 (fr) 1996-07-05
EP0853476B1 (fr) 2002-04-03

Similar Documents

Publication Publication Date Title
EP0946147B1 (fr) Composition apte au traitement de la fourbure equine
EP2301525B1 (fr) Préparation topique d'ibuprofène
KR101517494B1 (ko) 디클로페낙의 신규한 비수용성 국소 용액 및 이를 제조하는 과정
US4933184A (en) Menthol enhancement of transdermal drug delivery
ES2431330T3 (es) Composición de espuma en aerosol
Higgs et al. Inflammatory effects of prostacyclin (PGI2) and 6-oxo-PGF1α in the rat paw
JP5873439B2 (ja) ビタミンｄ類似体および溶媒と界面活性剤の混合物を含む皮膚組成物
US20030087885A1 (en) Pharmaceutical composition in the form of a gel or a solution based on dihydrotestosterone, process for preparing it and uses thereof
JP2008542353A (ja) ビタミン製剤
JP2002510336A (ja) 水溶性ケトプロフェン塩を含有する薬学的調製物及びその使用方法
JP5548275B2 (ja) ビタミンｄ類似体および共溶媒−界面活性剤混合物から成る医薬品組成物
AU3730799A (en) Preventives/remedies for skin diseases
JP2002504100A (ja) 肝腫瘍の治療方法およびそれに使用するための医薬組成物
JP2013515020A (ja) 溶媒混合物およびビタミンｄ誘導体から成る医薬品組成物または類似体
EP0853476B1 (fr) Preparation pharmaceutique contenant du nimesulide pour usage topique
Cooper et al. Mechanism of action of vasopressin on prostaglandin synthesis and vascular function in the isolated rat kidney: effect of calcium antagonists and calmodulin inhibitors.
KR101007161B1 (ko) 피부병 치료를 위한 아다팔렌의 용도
JPH03120230A (ja) 薬効成分の経皮吸収促進剤及び経皮吸収型製剤
WO2002007702A2 (fr) Formulation liposomique de propionate de clobetasol
US5817646A (en) Polar lipid composition of plant origin
ITMI20121965A1 (it) Composizione topica per il rilascio transepidermico o transdermico di paracetamolo
JPH11147826A (ja) 経皮吸収性の向上方法及び皮膚外用剤
CN120771114A (en) Baicalein-phospholipid complex nanoemulsion and preparation method and application thereof
JPH11209285A (ja) セラミド合成促進剤
Calvey et al. G. Seyffart, Drug Dosage in Renal Insufficiency© Kluwer Academic Publishers 1991

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 97191123.1

Country of ref document: CN

AK Designated states

Kind code of ref document: A2

Designated state(s): CA CN JP KR US

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): AT BE CH DE DK ES FI FR GB GR IE IT LU MC NL PT SE

WWE Wipo information: entry into national phase

Ref document number: 1997927313

Country of ref document: EP

AK Designated states

Kind code of ref document: A3

Designated state(s): CA CN JP KR US

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): AT BE CH DE DK ES FI FR GB GR IE IT LU MC NL PT SE

WWE Wipo information: entry into national phase

Ref document number: 1019980701516

Country of ref document: KR

ENP Entry into the national phase

Ref document number: 1998 504989

Country of ref document: JP

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: 2231118

Country of ref document: CA

Ref document number: 2231118

Country of ref document: CA

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 09029456

Country of ref document: US

121 Ep: the epo has been informed by wipo that ep was designated in this application
WWP Wipo information: published in national office

Ref document number: 1997927313

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 1019980701516

Country of ref document: KR

WWG Wipo information: grant in national office

Ref document number: 1997927313

Country of ref document: EP

WWR Wipo information: refused in national office

Ref document number: 1019980701516

Country of ref document: KR